专利号:WO-2025085030-A1 优先权日:2023-10-18 标 题:Synthesis of semisynthetic penicillin derivatives containing hydrazone-derived thiazolidine and imidazole ring 发明人:SARIPINAR EMIN; BURAN SUMEYYE 权利人:ERCIYES UNIV 摘要:The present invention relates to the novel semi-synthetic thiazolidine and imidazole penicillin, pharmaceutically acceptable derivatives thereof and their synthesis method that may cause biologically significant changes by the N-acylation reaction of 6-aminopenicillanic (6-APA) using new trisubstituted thiazolidine and imidazole acetyl chloride derivatives. The invention also relates to pharmaceutical compositions comprising these compounds and their use for therapeutic treatment in the human or animal body.
专利号:WO-2025085026-A1 优先权日:2023-10-18 标 题:Synthesis of semisynthetic penicillin derivatives containing hydrazone-derived thiazolidine and imidazole ring 发明人:SARIPINAR EMIN; BURAN SUMEYYE 权利人:T C ERCIYES UNIV 摘要:The present invention relates to the novel semi-synthetic thiazolidine and imidazole penicillin, pharmaceutically acceptable derivatives thereof and their synthesis method that may cause biologically significant changes by the N-acylation reaction of 6-aminopenicillanic (6-APA) using new trisubstituted thiazolidine and imidazole acetyl chloride derivatives. The invention also relates to pharmaceutical compositions comprising these compounds and their use for therapeutic treatment in the human or animal body.
专利号:US-2024336559-A1 优先权日:2021-10-06 标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids 发明人:OJIMA IWAO; HARANAHALLI KRUPANANDAN; DEL POETA MAURIZIO; GARG ASHNA 权利人:UNIV NEW YORK STATE RES FOUND 摘要:The present invention provides a compound having the structure: n n n n n n n n n n n n wherein n R 3 , R 4 , R 5 , R 6 , and R 7 are each independently, H, halogen, CN, —CF 3 , —OCF 3 , —NO 2 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, —OH, —OAc, —OR 13 , —COR 13 , —CH 2 OR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ; n R 9 , R 10 , R 11 , and R 12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, —OAc, —COR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ;n wherein each occurrence of R 13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 14 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 15 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, n n wherein when R 14 is methyl, R 15 is not methyl; n wherein at least one of R 9 , R 10 , R 11 , and R 12 is not H; n wherein at least one of R 3 , R 4 , R 5 , R 6 , and R 7 is not H.
专利号:US-10443047-B2 优先权日:2014-05-01 标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase 发明人:TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E 权利人:NOVOGY INC 摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.
专利号:US-12325678-B2 优先权日:2017-06-16 标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids 发明人:OJIMA IWAO; DEL POETA MAURIZIO; LAZZARINI CRISTINA; HARANAHALLI KRUPANANDAN; SUN YI 权利人:UNIV NEW YORK STATE RES FOUND 摘要:The present invention provides a compound having the structure: n nand use of the compound for inhibiting the growth of or killing.
专利号:US-2023364251-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.
1: Hashiguchi T, Ryu A, Itoyama T, Uchida K, Yamaguchi H. Study of the effective dose of a topical antifungal agent, omoconazole nitrate, on the basis of percutaneous pharmacokinetics in guinea-pigs and mice. J Pharm Pharmacol. 1997 Aug;49(8):757-61. doi: 10.1111/j.2042-7158.1997.tb06107.x. 39(6):825-7. doi: 10.1093/jac/39.6.825. 1(2):187-217. doi: 10.1128/cmr.1.2.187. 4: Itoyama T, Uchida K, Yamaguchi H, Fujita S. Therapeutic effects of omoconazole nitrate on experimental tinea pedis, an intractable dermatophytosis, in guinea-pigs. J Antimicrob Chemother. 1997 Sep;40(3):441-4. doi: 10.1093/jac/40.3.441. 41(5):395-402. doi: 10.1111/j.1348-0421.1997.tb01870.x. 76:264-73. doi: 10.1016/j.ejmech.2014.02.019. Epub 2014 Feb 11. 49(8):818-23. Japanese. 34(5 Pt 2):684-7. French. 22(14):4887-90. doi: 10.1016/j.bmcl.2012.05.070. Epub 2012 May 24.
合成参考文献
参考文献:10.1007/978-3-642-56567-0_5 参考文献:10.1007/978-3-031-15130-9_12 摘要:Rigopoulos D. Candidiasis. 2023. In: European Handbook of Dermatological Treatments. 参考文献:10.1007/978-981-97-5165-5_20 摘要:Ansari MD, Nouman, Mehandi R, Rana M, Rahisuddin. Bioactive Heterocyclic Analogs as Antifungal Agents: Recent Advances and Future Aspects. 2024. In: Advances in Antifungal Drug Development.